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Flashcards in PharmII_Exam2 Deck (105):
1

Which receptor does Diphenhydramine(benadryl) blocks?

It blocks H1 selectively

2

Name two drugs that can cause degranulation independent release of histamine?

Morphine
Tubocurarine

3

What two H receptors act in the CNS and Cardiovascular system?

H1 and H2

4

What is the antihistamine effect in the CNS?

Sedation
Depression
Anti-cholinergic effects
Stimulation (nervousness and restlessness)

5

What are the cardiovascular effects of histamine?

Decrease in blood pressure (H1 and H2)
Increase in heart rate (H2)

6

What are the bronchiole effect when antihistamine is present?

Bronchoconstriction (H1 receptors)

7

What are the GI effects of antihistamines?

H1 - intestinal contraction
H2 - Parietal cells secrete HCl

8

Describe the three parts in the wheal and flare response?

1. reddening of the area - vascular smooth muscle dilation
2. Edematous wheal - endothelium
3. Red irregular flare surrounding the wheal - axon reflex.

9

What is the hypersensitivity response?

1. Bronchoconstriction
2. Hypotension, tachycardia
3. Increase in capillary permeability
4. Edema

10

Give me an example of a popular physiologic antagonist?

Epinephrine

11

What are the three ways to block histamine reaction?

1. Physiological antagonist
2. Competitive antagonists
3. Inhibit the release

12

What is a summary of the 1st generation H1 antagonists?

More sedating
More autonomic receptor blockade.

13

Name the 4 categories of 1st generation antagonists?

1. Ethanolamines
2. Piperazine Derivatives
3. Alkylamines
4. Phenothiazines

14

What is so special about Ethanolamines?

More sedating.
More Anti-muscarinic actions
Motion sickness blockage

15

What separates the Piperazine Derivatives from the other H1 antagonists?

They are longer acting.

16

What is so special about Alkylamines and Phenothiazines?

They are more potent

17

What separates the 2nd generation drugs from the first?

They are less sedating.
They do not cross the BBB as easily or not at all

18

What are the two category of drugs found in 2nd gen antagonists?

Piperidines
Miscellaneous

19

What is Allegra used for?

Allergic rhinitis.
This is a 2nd generation H1 antagonists.

20

Does H1 1st gen or 2nd gen drugs last longer?

2nd gen drugs.

21

Which 2nd generation drug contains the most sedation out of the generation?

Zyrtec

22

What conditions are antihistamines really good for?

Allergic rhinitis
Urticaria

23

What condition is antihistamine not good for?

Bronchial asthma

24

Which generation do you give to ppl suffering from Allergic rhinitis and chronic Urticaria

2nd

25

What drug is the best for motion sickness?

Scopolamine.
Drugs like Dromazine and promethazine are used

26

T/F?
Antihistamines are used in sleeps aids?

True.
Sold OTC due to sedating effects.

27

What age does the child have to be to use anti-histamine?
What is the exception?

Over two years old.
Zyrtec can be used over 6 months.
Anti-histamines lead to seizures

28

Name the four topical agents for anti-histamines?

Olopatadine
Azelastine
Bepotastine
Levocabastine

29

What percentage of headaches do tension headaches compose of?

90%

30

How can primary headaches be classified as?

Tension
Migraine
Cluster

31

What drug do you use to treat gout?

NSAIDs

32

T/F?
Acetaminophen is a NSAID?

False
It has no anti-inflammatory properties

33

What are some adverse effects in NSAIDs?

Mild to moderate GI irritation
Hepatotoxicity
Nephrotoxicity

34

What are the three components found in prostanoids?

Prostaglandins
Thromboxanes
Prostacyclin

35

What occurs in phase I?

WBC bind to endothelial cells.
Become active, infiltrate

36

What occurs in phase 2?

WBC are activated for phagocytosis or lysosomal enzyme release

37

What occurs in phase 3?

Endothelial injury, tissue damage and inflammatory stimulus amp results.

38

Tell me about the enzyme COX 1?

It is constitutively expressed in all cells.
Housekeeping enzyme found in most cells

39

Tell me about COX2

It is an inducible enzyme.
You have to turn it on. Tissue damage will turn it on.

40

Tell me about COX-3

It is actually a splicing form of COX-1
It's function is unknown.

41

Prostanoid effect in the vascular system?

Thromboxane A2 = vasoconstriction
PGE2 and PGI2 = vasodilators

42

Prostanoid effect on GI?

Activate GI smooth muscle

43

Prostanoid effect on Airways?

PGs relax the airways
TXA2 and PGF2-alpha contracts

44

What happens if you block the COX1 mech in the GI?

You increase the amount of HCl that is released leading to ulcers.
Usually there is mucosal protection without this block.

45

What is the action of prostanoids in platelets?

PGE1 and PGEI2 inhibit the aggregation of platelets.
TXA2 stimulates the aggregation

46

What does a low dose of aspirin do in platelets?

It inhibits thromboxane A2 formation.
This is the cardioprotective effect

47

T/F?
Loop diuretics will get reduced with the use of prostanoids?

True

48

Effects of prostanoids in the eye?

It lowers IOP

49

T/F?
The effects of aspirin are reversible?

False.
They are irreversible. Its effects are longer than that predicted by its 1/2 life.
The COX enzyme must be re-synthesized to return normal function.

50

Symptomatic relief is provided by NSAIDs in which of the three categories?

Anti-inflammatory

51

What percentage does NSAIDs reduce the chances of getting colon cancer?

By 50%

52

Tell me about the relation COX-2 have with thrombotic events?

COX 2 does not mess with TXA2
COX2 does suppress PGI2
WHen u suppress PGI2, u lead to an activation of platelets and cause potential thrombotic events.

53

T/F?
THe metabolism of aspirin is saturable?

True
ANother drug that is saturable is phenytoin

54

How long is a patient told not to take NSAIDs before surgery?

7 days.
Because it takes 8-11 days for platelets to regenerate.

55

Which drug is Reye's syndrome linked to?

Aspirin
It is given to children with viral infections and fever.
Instead give the child acetaminophen or ibuprofen.

56

T/F?
It is perfectly OK to use aspirin in gout?

False!!!
Aspirin does not eliminate uric crystals

57

What are some adverse effects of aspirin intoxication?

Headache
Dizziness
Tinnitus
Hearing loss
................

58

Which drug is more potent than aspirin but not more efficacious?

Indocin

59

What is so special about Clinoril?

Half as potent as Indocin.
Suppresses familial intestinal polyposis
INhibit the development of colon, breast, and prostate cancer.

60

Which drug is better tolerated than aspirin?

Tolectin
It is also just as efficacious.
It is indicated for use for rheumatic disease including the juvenile form

61

What drug can be used in place of opioids like morphine and is as efficacious for postoperative pain?

Toradol

62

T/F?
U can take ibuprofen while breastfeeding?

False

63

Which propionic acid has an increased Cardiovascular risk compared to a placebo with long term usage?

Naproxen

64

Which propionic acid derivative is the most potent?

Ketoprofen

65

Why do we use Cox2?

To prevent adverse GI effects and platelet actions

66

Which cylcooxygenase inhibitor class have a black box warning?

all NSAIDs that inhibit COX-2 (nonselective COx inhibitors and COX-2 selective agents),
except for aspirin - has cardioprotective features

67

Which two cox inhibitors were pulled from the market due to cardiovascular effects?

Vioxx
Bextra

68

T/F?
Acetaminophen has peripheral effects?

False
It does not inhibit peripheral COX enzymes. Does not inhibit platelet aggregation.
No severe GI problems.

69

What population is acetaminophen good in?

Elderly
Young children

70

How do you treat toxicity from Acetaminophen?

Gastric lavage
Addition of sulfhydryl compounds to replenish glutathione.
N-actylcysteine

71

What is the therapeutic approach to treat gout?

1. Reduce inflammation
2. Increase the elimination of Uric acid
3. Decrease the production of Uric acid

72

What is the function of colbenemid in gout?

Reduce the pain and inflammation.

73

MOA of colbenemd?

It binds to and blocks tubulin.
prevents its polymerization preventing leukocyte migration and phagocytosis of uric acid crystals.

74

which two classes of NSAIDs don't work in gout?

Salicylates and tolectin

75

Which NSAID is the best to use in gout?

Indocin.
Inhibits phagocytosis of urate crystals.

76

MOA of allopurinol?

Inhibits xanthine oxidase which Prevents uric acid biosynthesis

77

Analgesic efficacy is mediated via which receptor?

Mew receptors

78

Which area in the brain contains a high concentration of
opioid receptors that facilitate feelings of euphoria.

Nucleus accumbens

79

T/F?
Opioid withdrawal is life-threatening?

False
Alcohol and morphine is life threatening.

80

I should never give a patient an opioid due to its dependcence levels!

Despite the propensity for abuse and the development of dependence, these drugs should never be withheld as analgesics.

81

Which pain reacts well to opiates?

Nociceptive pain.
Stimulation of nociceptors along intact neural pathways.

82

Which pain does opiates react poorly to?

Neuropathic pain.
May need to increase the dose to have an effect.

83

T/F?
Ascending pain pathway- Opioids inhibit the ascending pathway at the dorsal horn (spinal) and at the thalamus
(supraspinal).

True

84

Are the kappa receptors found in ascending or descending pathway?

Desceinding.
They work oppositely form the mew receptor

85

Stimulation of descending pathway will do what?

Inhibit the ascending pathway.

86

When sensory input is high, is there more or less respiratory distress?

Less!!!
Ex: someone is injured; the sensory input is gonna be mad high. As the pain goes away, the sensory input will increase.

87

Cimetidine

H2 antagonist
used for their ability to reduce acid secretions

88

T/F?
Chronic postoperative pain or pain from inflammation is well-controlled by NSAIDs?

True

89

What does PGI2 do?

Normally suppresses platelet activation, so inhibiting it can cause
platelet over activation aka Thrombotic events. (this is why Vioxx and Bextra were withdrawn)

90

T/F?
COX-2 selective agents and p-aminophenol derivatives are less harmful to the stomach because COX-1 is responsible for buffering stomach acid.

True

91

Secondary use for indocin?

closure of patent ductus arteriosis in premature babies

92

Diflusnisal


• Dental and cancer pain
• Better anti inflammatory than aspirin
• Used as an analgesic with less auditory, GI, and platelet side effects.

93

T/F?
It is OK to use acetaminophen on any kind of gout?

False
Due to the fact that acetaminophen has no anti-inflammatory properties.

94

Which agents are better tolerated than aspirin and indomethacin

Propionic acids
Efficacy is similar to the sals.
The sals are cheaper

95

Peroxicam?

Advantage is long 1/2 life so only single daily dose

96

Give me two examples of uricosuric agents?

Probenecid
Sulfinpyrazone

97

How long do you wait after a gouty attack to start a patient on probenecid and sulfinpyrazone?

Wait 2-3 weeks.
U use these drugs when patient has had several acute attacks or if urate levels are very high and an attack is inevitable.

98

Febuxostat

A new drug that is more effective at lowering serum ureate levels than allopurinol.
THere are hepatic problems causing death.

99

Name two examples of xanthine oxidase inhibitors?

Allopurinol
Febuxostat

100

Diclofenac

Relatively high potency agent with selectivity for COX 2

101

Meloxicam

Selective for COX 2.
Comparable efficacy with less GI effects.

102

Etodolac

Slightly selective for COX 2
Useful for post op pain.

103

What is an AE for etodolac?

Temporary renal problems.

104

Celebrex

Similar efficacy as other NSAIDs with fewer adverse GI effects
Pfizer has said that the prothrombotic effects seen with Vioxx don't happen at therapeutic doses of celebrex.

105

When do you start a patient on prophylactic treatment for migraines?

If patient experiences more than three migraine attacks per month